Tag: M.W=100-150

Hameed P, Shahul; Patil, Vikas; Solapure, Suresh; Sharma, Umender; Madhavapeddi, Prashanti; Raichurkar, Anandkumar; Chinnapattu, Murugan; Manjrekar, Praveena; Shanbhag, Gajanan; Puttur, Jayashree; Shinde, Vikas; Menasinakai, Sreenivasaiah; Rudrapatana, Suresh; Achar, Vijayashree; Awasthy, Disha; Nandishaiah, Radha; Humnabadkar, Vaishali; Ghosh, Anirban; Narayan, Chandan; Ramya, V. K.; Kaur, Parvinder; Sharma, Sreevalli; Werngren, Jim; Hoffner, Sven; Panduga, Vijender; Kumar, C. N. Naveen; Reddy, Jitendar; Kumar KN, Mahesh; Ganguly, Samit; Bharath, Sowmya; Bheemarao, Ugarkar; Mukherjee, Kakoli; Arora, Uma; Gaonkar, Sheshagiri; Coulson, Michelle; Waterson, David; Sambandamurthy, Vasan K.; de Sousa, Sunita M. published the artcile< Novel N-Linked Aminopiperidine-Based Gyrase Inhibitors with Improved hERG and in Vivo Efficacy against Mycobacterium tuberculosis>, Safety of 5-Fluoropyridine-2,3-diamine, the main research area is aminopiperidinyl quinolone naphthyridone Mycobacterium tuberculosis bactericide DNA gyrase inhibitor.

DNA gyrase is a clin. validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clin. value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochem. studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis (e.g., compound I).

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Safety of 5-Fluoropyridine-2,3-diamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zheng, Ke; Iqbal, Sarah; Hernandez, Pamela; Park, HaJeung; LoGrasso, Philip V.; Feng, Yangbo published the artcile< Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives>, Electric Literature of 56622-54-9, the main research area is aminopyrazole JNK3 enzyme inhibitor preparation structure neurodegeneration.

The c-jun N-terminal kinase 3 (JNK3) is expressed primarily in the brain. Numerous reports have shown that inhibition of JNK3 is a promising strategy for treatment of neurodegeneration. The optimization of aminopyrazole-based JNK3 inhibitors with improved potency, isoform selectivity, and pharmacol. properties by structure-activity relationship (SAR) studies utilizing biochem. and cell-based assays, and structure-based drug design is reported. These inhibitors had high selectivity over JNK1 and p38α, minimal cytotoxicity, potent inhibition of 6-OHDA-induced mitochondrial membrane potential dissipation and ROS generation, and good drug metabolism and pharmacokinetic (DMPK) properties for iv dosing. 26n was profiled against 464 kinases and was found to be highly selective hitting only seven kinases with >80% inhibition at 10 μM. Moreover, 26n showed good solubility, good brain penetration, and good DMPK properties. Finally, the crystal structure of 26k in complex with JNK3 was solved at 1.8 Å to explore the binding mode of aminopyrazole based JNK3 inhibitors.

Journal of Medicinal Chemistry published new progress about Drug metabolism. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Electric Literature of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hu, Ziwei; Banothu, Janardhan; Beesu, Mallesh; Gustafson, Collin J.; Brush, Michael J. H.; Trautman, Kathryn L.; Salyer, Alex C. D.; Pathakumari, Balaji; David, Sunil A. published the artcile< Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides>, Computed Properties of 56622-54-9, the main research area is dihydropyridine quinolone carboxamide synthesis SAR TLR2 vaccine adjuvant.

Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-N-(pyridin-3-ylmethyl)-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxamide as a TLR2 agonist. Preliminary structure-activity relationship studies on the carboxamide moiety led to the identification of analogs that induce chemokines and cytokines in a TLR2-dependent manner. These results represent new leads for the development of vaccine adjuvants.

ACS Medicinal Chemistry Letters published new progress about Chemokines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Computed Properties of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Stavber, Stojan; Zupan, Marko published the artcile< Reactions of cesium fluoroxysulfate with pyridine>, Name: 3-Chloro-2-methoxypyridine, the main research area is pyridine fluorination cesium fluoroxysulfate solvent effect.

Pyridine readily reacts with CsSO4F in various solvents at room temperature producing a mixture of up to three products (2-fluoropyridine, 2-pyridyl fluorosulfonate and 2-chloro or 2-alkoxypyridine), their distribution strongly depending on the solvent used. Reaction of 3-chloropyridine with CsSO4F in methanol leads regioselectively to 2-methoxy-3-chloropyridine, while 3-methylpyridine was converted into 2-methoxy-3-Me and 2-methoxy-5-methylpyridine in a 2:1 relative ratio.

Tetrahedron Letters published new progress about Fluorination. 13472-84-9 belongs to class pyridine-derivatives, and the molecular formula is C6H6ClNO, Name: 3-Chloro-2-methoxypyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Bin; Xu, Zhi-Qiang; Xu, Ying-Bo; Yong, Guo-Ping published the artcile< Effects of substituent groups on the crystal structures and luminescence properties of zero-/two-dimensional Zn(II) complexes>, Electric Literature of 350-03-8, the main research area is crystal structure zinc imidazopyridine polymeric monomeric preparation luminescence.

The 3-position substituted imidazo[1,2-a]pyridine ligands C7H4N2Cl-2-(CH:CHC(:O)R)-3 (L1, R = 3-pyridinyl) and (HL2, R = COOH) were facilely synthesized, and used for construction of two novel luminescent Zn(II) complexes, [ZnCl2(L1)2] (1) and [Zn(L2)2]n (2). Single-crystal x-ray diffraction anal. shows that 1 has a zero-dimensional structure, whereas, 2 possesses a two-dimensional polymeric network with rhombic grid motifs. The structural differences between 1 and 2 should be determined by the different substituent groups adjacent to the carbonyl groups of the 3-position substituted imidazo[1,2-a]pyridine ligands. Complex 1 reveals a red shifted emission band, compared to free L1 ligand, whereas, 2 displays a similar emission spectrum as the free HL2 ligand. Such results are also ascribed to substituent group effects and corresponding structural differences.

Inorganic Chemistry Communications published new progress about Crystal structure. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Electric Literature of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cai, Pengfei; Gao, Zhan; Yin, Xinchi; Luo, Yuanqing; Zhao, Xiaoyong; Pan, Yuanjiang published the artcile< facile enantioseparation and recognition of mandelic acid and its derivatives in self-assembly interaction with chiral ionic liquids>, Synthetic Route of 3796-23-4, the main research area is enantioseparation mandelic acid derivatives self assembly chiral ionic liquids; chiral separation; coprecipitation; ionic liquids; mandelic acid.

Mandelic acid and its derivatives are important medical intermediates in the pharmaceutical industry. Different stereoisomers exhibited distinct biol. properties to human bodies. Given that, enantioselective recognition and separation of mandelic acid are of great importance. In this study, four novel different types of chiral ionic liquids bearing designed functional groups were synthesized and successful enantioselective precipitation with mandelic acid and its derivatives That is, (R, R)-chiral ionic liquid 1 can coprecipitated with S-mandelic acid and its derivatives was observed In addition, good correlation coefficient is achieved by using electrospray mass spectrum at neg. ion pattern for quick anal. of the enantioselective precipitation, which could be served as a method of enantioselective recognition. The possible intermol. interactions are established after systematical studies by NMR spectroscopy and DFT calculations

Journal of Separation Science published new progress about Chiral resolution. 3796-23-4 belongs to class pyridine-derivatives, and the molecular formula is C6H4F3N, Synthetic Route of 3796-23-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jackson, Matthew Irick published the artcile< Macronutrient Proportions and Fat Type Impact Ketogenicity and Shape the Circulating Lipidome in Dogs>, Application In Synthesis of 93-60-7, the main research area is macronutrient fat ketogenicity lipidome circulation dog; canine; ketosis; lipidome; macronutrients; metabolome.

Many physiol. processes including ketogenesis are similar in dogs and humans, but there is little information available on the effect of carbohydrate restriction in dogs. Here, the ketogenicity and serum metabolic profiles of dogs were assessed after they had consumed high carbohydrate (HiCHO); high protein, low carbohydrate (PROT_LoCHO); or high fat, low carbohydrate (FAT_LoCHO) foods. Thirty-six dogs were fed HiCHO for 4 wk, then randomized to PROT_LoCHO or FAT_LoCHO for 5 wk. Dogs then crossed over to the other food for an addnl. 5 wk. Generally, reduction of dietary carbohydrate by replacement with either protein or fat increased the energy required to maintain body weight, and fat had a greater effect. Postabsorptive energy availability derived mainly from glucose and triglycerides with HiCHO, from gluconeogenic amino acids and fatty acids with PROT_LoCHO, and from fatty acids and β-hydroxybutyrate with FAT_LoCHO. This study demonstrated that the reduction of carbohydrate in canine foods is potentially beneficial to dogs based on improvements in metabolism and supports the use of low-carbohydrate foods as safe and effective for healthy adult dogs.

Metabolites published new progress about Absorption. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Application In Synthesis of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lengacher, Raphael; Wang, Youchao; Braband, Henrik; Blacque, Olivier; Gasser, Gilles; Alberto, Roger published the artcile< Organometallic small molecule kinase inhibitors - direct incorporation of Re and 99mTc into Opaganib>, Quality Control of 3731-53-1, the main research area is prostate cancer opaganib bioorganometallic complex anticancer mol theranostics.

[(η5-Cp)ReI(CO)3] was incorporated into the kinase inhibitor Opaganib. The resulting bioorganometallic complex showed a similar anti-cancer activity to Opaganib against PC-3 cancer cells. The IC50 value for the kinase SK2 is 30x higher than that of Opaganib. The 99mTc homolog was synthesized, completing a matched-pair for mol. theranostics.

Chemical Communications (Cambridge, United Kingdom) published new progress about Antitumor agents. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Biehl, Zulfe Urbano published the artcile< Review of the scientific and technological literature of fungicides in tannery industry: reducing the use and increasing the efficiency of fungicides in the leather industry>, Product Details of C5H4NNaOS, the main research area is fungicide biocide phylogenetics biodeterioration ergosterol azoles microbial fungi.

One of the main challenges of the tannery industry chain is to reduce the use of biocides and restricted substances and at the same time increase efficiency with the available products. Such conduct must permeate suppliers and the tanneries in order to obtain better results, diminish the biocide resistance dissemination, optimize costs and be ecol. friendly. In this sense, we present herein an updated review and discussion of the scientific and technol. literature on the aspects involving the action of fungicides in tannery industry and how the application of this knowledge can reduce application of biocides and restricted substances in the tanning process. We have organized a review by consulting the databases PUBMED, Web of Science, Science direct, and all literature with excellence scientific support available. The review focused on: (i) Fungal diversity involved in wet-blue biodeterioration; (ii) Mechanisms of action of fungicides; (iii) Fungicide combinations to enhance activity; (iv) Fungal mechanisms of resistance and the known causes of resistance emergence. As a result of this study we are able to track the fungal phylogenetics (and relationship) responsible for leather biodeterioration enabling a guiding strategy for fungal biocide application. Moreover, understanding of the mechanisms of action and interaction between mols. can determines the extent of the biocides inhibitory effect in different fungal species. Fungicide effect could vary, and such information corroborates with the idea that even in the same species the interaction of the different mols. may vary, possibly due to variation in cytochrome protein. For example, the most accepted mechanism of action of azoles is the inhibition of synthesis of or direct interaction with ergosterol (present in all fungi). Considering that the target is always the same, a question arise, how do the distinct azoles present different activities upon fungal strains. As result of this study we show that structural differences will influence the higher or lower interaction of the azole functional group and consequently the activity. The appropriated knowledge of the mechanisms by which microbial cells might develop resistance, highlights the need for an improved understanding of the reasons for their emergence and greater attention to methods that can be used to prevent and control them. In this sense, a successful combination of biocide mols. enhances a synergetic effect, avoiding fungal mechanisms of resistance and reduces dosage of each compound, being effective against a variety of fungi.

Journal of AQEIC published new progress about Alternaria. 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, Product Details of C5H4NNaOS.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ye, Shanghui; Wu, Congjin; Gu, Pengfei; Xiang, Tai; Zhang, Senyu; Jing, Tongtong; Wang, Shi; Yang, Xiaodi; Li, Yonghua; Huang, Wei published the artcile< A benzoindole-cored building block for deep blue fluorescent materials: synthesis, photophysical properties, and applications in organic light-emitting diodes>, Formula: C6H8N2, the main research area is benzoindole cored blue fluorescent material organic light emitting diode; LED organic benzoindole cored blue fluorescent material; electroluminescent device organic benzoindole cored blue fluorescent material.

Deep blue fluorescent materials are crucial in the commercialization of organic light-emitting diodes (OLEDs) for full-color displays or solid-state lighting sources. Aromatic ring compounds based on a newly designed 2-(pyridine-4-yl)-3-phenyl-1H-benzo[g]indole core, were synthesized, on which donor (D) and acceptor (A) groups are bonded in a Y-typed configuration, forming a D-π-A-π-D structure. The electronic structure and photophys. properties were explored, as well as the applications in the blue OLEDs. Multi-state couplings exist between the D-π-A-π-D 3 moieties, resulting in high luminescence quantum yield ≤76.1% peaking at ∼410 nm, and depressed efficiency roll-off at high luminance. The deep blue OLEDs based on CzCNBPyIp emitter exhibits stable emission peaking at 416 nm with negligible efficiency roll-off at high luminance range of 1,000-10,000 cd m-2, and corresponding CIEx,y = (0.162, 0.085) and maximum EQE = 2.6%, making it among the highest performance solution processed deep blue fluorescent devices. This work provides an alternative method for the deep blue fluorescent materials design toward solution processing OLEDs.

Journal of Materials Chemistry C: Materials for Optical and Electronic Devices published new progress about Electron acceptors. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem